Search Result
Results for "
Lenalidomide hemihydrate
" in MedChemExpress (MCE) Product Catalog:
3
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-A0003B
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CC-5013 hemihydrate
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Ligands for E3 Ligase
Molecular Glues
Apoptosis
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Cancer
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Lenalidomide hemihydrate (CC-5013 hemihydrate), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hemihydrate is an orally active immunomodulator. Lenalidomide hemihydrate (CC-5013 hemihydrate) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hemihydrate (CC-5013 hemihydrate) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
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- HY-W076696
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Ligands for E3 Ligase
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Cancer
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Lenalidomide-4-OH is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-4-OH can be connected to the ligand for protein by a linker to form PROTAC.
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- HY-W072954
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Ligands for E3 Ligase
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Cancer
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Lenalidomide-5-Br is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-5-Br can be connected to the ligand for protein by a linker to form PROTAC .
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- HY-W077589
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Ligands for E3 Ligase
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Cancer
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Lenalidomide-5-aminomethyl hydrochloride is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-5-aminomethyl hydrochloride can be connected to the ligand for protein by a linker to form PROTAC
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- HY-138881
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Ligands for E3 Ligase
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Cancer
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Lenalidomide-6-F is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-6-F can be connected to the ligand for protein by a linker to form PROTAC .
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- HY-145461
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5-Hydroxy Lenalidomide
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Others
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Others
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Hydroxy lenalidomide (5-Hydroxy lenalidomide) is a metabolite of lenalidomide that is present as a minor component in plasma and excreta, accounting for less than 5% of the total radioactivity, following oral administration of lenalidomide in healthy male subjects.
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- HY-W077589A
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Ligands for E3 Ligase
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Cancer
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Lenalidomide-5-aminomethyl is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-5-aminomethyl can be connected to the ligand for protein by a linker to form PROTAC .
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- HY-138882A
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Ligands for E3 Ligase
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Cancer
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Lenalidomide-4-aminomethyl hydrochloride is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-4-aminomethyl hydrochloride can be connected to the ligand for protein by a linker to form PROTAC
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- HY-138882
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Ligands for E3 Ligase
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Cancer
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Lenalidomide-4-aminomethyl is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-4-aminomethyl can be connected to the ligand for protein by a linker to form PROTAC .
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- HY-161675
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Lenalidomide-5-bromopentanamide is an E3 ligase ligand-linker conjugate in PROTAC ATR degrader-2 (HY-161615), and consists of a CRBN ligand Lenalidomide (HY-A0003) and a linker 5-Bromopentanoyl chloride (HY-43538). Lenalidomide-5-bromopentanamidecan be used for synthesis of PROTACs .
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- HY-A0003R
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Ligands for E3 Ligase
Molecular Glues
Apoptosis
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Inflammation/Immunology
Cancer
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Lenalidomide (Standard) is the analytical standard of Lenalidomide. This product is intended for research and analytical applications. Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
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- HY-133144
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Ligands for E3 Ligase
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Cancer
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Lenalidomide-OH is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-OH can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC BTK degrader SJF620 (HY-133137) .
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- HY-132248
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Lenalidomide 5'-amine
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TNF Receptor
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Inflammation/Immunology
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C5 Lenalidomide (Lenalidomide 5'-amine) is a thalidomide analog and is a potent inhibitor of TNF-alpha production (IC50=100 μM in LPS stimulated human PBMC) .
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- HY-131318
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Ligands for E3 Ligase
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Cancer
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Lenalidomide-I (Compound 72), an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, is used in the recruitment of CRBN protein. Lenalidomide-I can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC BET degrader QCA570 (HY-112609) .
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- HY-160241
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Lenalidomide-C5-acid is the Lenalidomide-based E3 ligase ligand-linker conjugate used in the recruitment of CRBN protein. Lenalidomide-C5-acid can be used to synthesize PROTACs .
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- HY-43722
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Ligands for E3 Ligase
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Cancer
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Lenalidomide-Br (Compound 41) is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-Br can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC STAT3 degrader SD-36 (HY-129602) .
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- HY-161451
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Lenalidomide nonanedioic acid is a conjugate of the E3 ligase ligand and linker of LHF418 (HY-161450). Lenalidomide nonanedioic acid can be used as a key intermediate for the synthesis of intact PROTACs molecules .
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- HY-169362
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Lenalidomide-Pip-butyn is Lenalidomide (HY-A0003)-based E3 ligase ligand-linker conjugate, and is used in the recruitment of CRBN protein. Lenalidomide-Pip-butyn can be connected to the ligand for protein to form PROTACs, such as the PROTAC STAT3 degrader SD-436 (HY-169360) .
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- HY-A0003
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Lenalidomide
Maximum Cited Publications
39 Publications Verification
CC-5013
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Ligands for E3 Ligase
Molecular Glues
Apoptosis
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Inflammation/Immunology
Cancer
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Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
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- HY-A0003A
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CC-5013 hydrochloride
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Ligands for E3 Ligase
Molecular Glues
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Inflammation/Immunology
Cancer
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Lenalidomide hydrochloride (CC-5013 hydrochloride), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hydrochloride is an orally active immunomodulator. Lenalidomide hydrochloride (CC-5013 hydrochloride) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hydrochloride (CC-5013 hydrochloride) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
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- HY-132856
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Lenalidomide-C5-amido-Boc is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C5-amido-Boc can be connected to the ligand for protein by a linker to form PROTAC .
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- HY-161129
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Lenalidomide 4'-PEG2-amine dihydrochloride is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide 4'-PEG2-amine dihydrochloride can be connected to the ligand for protein by a linker to form PROTAC .
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- HY-161128
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Lenalidomide 4'-PEG1-amine dihydrochloride is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide 4'-PEG1-amine dihydrochloride can be connected to the ligand for protein by a linker to form PROTAC .
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- HY-161130
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Lenalidomide 4'-PEG3-amine dihydrochloride is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide 4'-PEG3-amine dihydrochloride can be connected to the ligand for protein by a linker to form PROTAC .
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- HY-161134
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Lenalidomide 4'-PEG2-azide is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide 4'-PEG2-azide can be connected to the ligand for protein by a linker to form PROTAC .
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- HY-133139
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Lenalidomide-PEG1-azide is a E3 ligase lgand-linker conjugate. Lenalidomide-PEG1-azide incorporates the Lenalidomide based cereblon ligand and a linker.?Lenalidomide-PEG1-azide?can be used to design a PROTAC BRD4 Degrader-2 (HY-133136) . Lenalidomide-PEG1-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-161133
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Lenalidomide 4'-PEG1-azide (Compound 4g) is a lenalidomide-derived azide. Lenalidomide 4'-PEG1-azide incorporates the Lenalidomide based cereblon ligand and a linker. Lenalidomide 4'-PEG1-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups. .
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- HY-122725B
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Lenalidomide-C5-NH2 hydrochloride is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C5-NH2 can be connected to the ligand for protein by a linker to form PROTACs, such as MDM2 PROTAC degrader .
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- HY-169181
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- HY-130982
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Lenalidomide-PEG3-iodine is a synthesized E3 ligase ligand-linker conjugate that incorporates the Lenalidomide based cereblon ligand and a 3-unit PEG linker. Lenalidomide-PEG3-iodine can be used in the synthesis of a series of PROTACs, such as SJF620 (HY-133137). SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM .
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- HY-161538
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- HY-122725A
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Lenalidomide-C5-NH2 is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C5-NH2 can be connected to the ligand for protein by a linker to form PROTACs, such as MDM2 PROTAC degrader .
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- HY-163647
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Lenalidomide-COCH-PEG2-azido is a synthesized E3 ligase ligand-linker conjugate that incorporates the Lenalidomide (HY-A0003) based cereblon ligand and a linker. Lenalidomide-COCH-PEG2-azido can be used in the synthesis of PROTAC AKR1C3 degrader-1 (HY-163609) .
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- HY-A0003S
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CC-5013-d5
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Isotope-Labeled Compounds
Ligands for E3 Ligase
Molecular Glues
Apoptosis
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Inflammation/Immunology
Cancer
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Lenalidomide-d5 is deuterium labeled Lenalidomide. Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells[1][2].
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- HY-139340
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Others
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Others
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Photo-lenalidomide-acid (compound 3) is a photacts consist of a ligand for an E3 ligase, a photoswitch, and a ligand for a protein of interest and enable optical control of protein degradation .
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- HY-W797329
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Ligands for E3 Ligase
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Cancer
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(3S)Lenalidomide-5-Br is a ligand for E3 ubiquitinase. (3S)Lenalidomide-5-Br can be used to synthesize PROTAC Cbl-b-IN-1 (HY-159608) .
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- HY-W777286
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- HY-139563
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Others
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Others
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Lenalidomide-C10-OH (6a) is an intermediate in the synthesis of INY-03-041 .
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- HY-161131
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E3 Ligase Ligand-Linker Conjugates
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Inflammation/Immunology
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Lenalidomide 4'-alkyl-C3-azide (compound 4a) is a click chemical modified Lenalidomide (HY-A0003) that can be used to synthesize PROTACs. Lenalidomide is an orally active immunomodulator and a ligand for the ubiquitin E3 ligase cereblon (CRBN). Lenalidomide 4'-alkyl-C3-azide contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition reactions (SPAAC) can also occur with molecules containing DBCO or BCN groups .
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- HY-129608
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Cereblon ligand-linker Conjugate
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Lenalidomide-acetylene-C5-COOH (compound 43; Cereblon ligand-linker Conjugate) is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-acetylene-C5-COOH can be connected to the ligand for protein by a linker to form PROTAC . Lenalidomide-acetylene-C5-COOH is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-W259932
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Ligands for E3 Ligase
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Cancer
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Lenalidomide 5'-piperazine is a functionalized cerebellar ligand for PROTAC development that binds an E3 ligand to terminal piperazine for subsequent chemical reactions to produce a protein deactivator with a rigid linker .
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- HY-130683
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Lenalidomide-propargyl-C2-NH2 hydrochloride incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase, and a linker. Lenalidomide-propargyl-C2-NH2 hydrochloride can be used to design the PROTAC MD-224 (HY-114312) . Lenalidomide-propargyl-C2-NH2 (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-168272
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(3S)Lenalidomide-piperazine-C-piperidine is an E3 ubiquitinase ligand + linker conjugate (E3 Ligase Ligand-Linker Conjugates). (3S)Lenalidomide-piperazine-C-piperidine can be used to synthesize PROTAC PROTAC ER Degrader-11 (HY-168270) .
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- HY-163964
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- HY-159145
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-
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- HY-168298
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Lenalidomide-6-F-piperidine-C2-Pip-C-COOH is a linker and E3 ligase ligand for PROTAC BTK Degrader-5 (HY-155072) and can be used in malignant lymphoma research .
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- HY-156700
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PROTAC Linkers
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Cancer
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Lenalidomide-acetylene-Br is a PROTAC Linker taht makes up HJM-561 (HY-156698). HJM-561 is a potent, selective, and orally active EGFR PROTAC to inhiibit Osimertinib (HY-15772)-resistant EGFR triple mutations.
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- HY-130682
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Lenalidomide-propargyl-C2-amido-Ph-NH2 hydrochloride incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase and a linker. Lenalidomide-propargyl-C2-amido-Ph-NH2 hydrochloride can be used to design the PROTAC MD-224 (HY-114312) . Lenalidomide-propargyl-C2-amido-Ph-NH2 (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-157566
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Ligands for E3 Ligase
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Cancer
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Lenalidomide 5'-piperazine-4-methylpiperidine hydrochloride is a functionalized cerebellar ligand for PROTAC development, combining E3 ligand and terminal piperidine for subsequent chemical reactions. A protein degradant with a rigid connector is generated .
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- HY-A0003S2
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CC-5013-13C5,15N
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Ligands for E3 Ligase
Apoptosis
Molecular Glues
Isotope-Labeled Compounds
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Inflammation/Immunology
Cancer
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Lenalidomide- 13C5, 15N is 15N and 13C labeled Lenalidomide (HY-A0003). Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
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- HY-161132
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E3 Ligase Ligand-Linker Conjugates
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Others
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Lenalidomide 4'-alkyl-C5-azide is a functionalized cerebellar ligand for PROTAC development that contains an E3 ligand and an alkyl LC5 ligand with terminal azides that can be coupled to a target protein ligand .
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- HY-159618
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(3S)Lenalidomide-5-Pip-C-Pip-2C-Pip is an E3 Ligase Ligand-Linker Conjugate. (3S)Lenalidomide-5-Pip-C-Pip-2C-Pip can be used to synthesize PROTAC Cbl-b-IN-1 (HY-159608) .
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- HY-115446A
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Cereblon ligand 1 hydrochloride; E3 ligase Ligand-Linker Conjugates 32 hydrochloride
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Lenalidomide-C4-NH2 hydrochloride is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C4-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTAC (Compound 24), which has IC50s of 0.98 nM and 13.7 nM in inhibition of RS4;11 and MOLM-13 acute leukemia cell lines growth, respectively .
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- HY-159608
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PROTACs
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Cancer
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PROTAC Cbl-b-IN-1 (compound 64) is a PROTAC targeting Cbl-b. PROTAC Cbl-b-IN-1 is composed of PROTAC target protein ligand Cbl-b-IN-21 (HY-159615), PROTAC Linker Cbz-Pip-2C-Pip-C-Pip (HY-159617) and E3 ubiquitin ligase ligand (3S) Lenalidomide-5-Br (HY-W797329), where the E3 ubiquitin ligase ligand + Linker conjugate is (3S) Lenalidomide-5-Pip-C-Pip-2C-Pip (HY-159618) [1] .
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- HY-133137
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PROTACs
Btk
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Cancer
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SJF620 is a PROTAC connected by ligands for Cereblon and Btk with a DC50 of 7.9 nM. SJF620 contains a Lenalidomide analog for recruiting CRBN .
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- HY-133137A
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PROTACs
Btk
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Cancer
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SJF620 hydrochloride is a PROTAC connected by ligands for Cereblon and Btk with a DC50 of 7.9 nM. SJF620 contains a Lenalidomide analog for recruiting CRBN .
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- HY-157767
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PROTACs
ATM/ATR
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Cancer
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Abd110 (compound 42i) is a Lenalidomide-based PROTAC ATR kinase degrader. Abd110 selectively decreases ATR and phospho-ATR without affecting related kinases ATM and DNA-PKcs .
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- HY-130988A
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GDC-0068-NH2 dihydrochloride; RG7440-NH2 dihydrochloride
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Ligands for Target Protein for PROTAC
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Cancer
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Ipatasertib-NH2 dihydrochloride is a ligand for target protein AKT for PROTAC (INY-03-041). INY-03-041 is composed of Ipatasertib-NH2, a ten-hydrocarbon linker, and a CRBN ligand Lenalidomide for E3 ubiquitin ligase .
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- HY-120084
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Casein Kinase
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Cancer
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BTX161, a thalidomide analog, is an effective CKIα degrader. BTX161 mediates human AML cell CKIα degradation more effectively than lenalidomide and activates the DNA damage response (DDR) and p53, while stabilizing p53 antagonist MDM2.
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- HY-163962
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PROTACs
Btk
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Inflammation/Immunology
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L18I is a PROTAC targeting Btk that can reduce inflammation in autoimmune diseases such as lupus erythematosus induced by BM12 splenocytes. L18I is composed of PROTAC target protein ligand IBT6A (HY-13036A) (red part), PROTAC Linker Propargyl-PEG3-alcohol (HY-41921) (balck part) and E3 ubiquitin ligase ligand Lenalidomide-Br (HY-43722) (blue part), of which the active control of the target protein ligand is IBT6A-CO-ethyne (HY-163963), and the conjugate of E3 ubiquitin ligase ligand + Linker is Lenalidomide-C3-PEG3-N3 (HY-163964) [1] .
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- HY-156591
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PROTACs
Mixed Lineage Kinase
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Others
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PROTAC MLKL Degrader-1 (Compound 36) is a PROTAC degrader of MLKL, with a Dmax >90%. PROTAC MLKL Degrader-1 contains modified CRBN ligands, linker and Lenalidomide (HY-A0003)-linker fragments. PROTAC MLKL Degrader-1 abrogates cell death in a TSZ model of necroptosis.
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- HY-155075
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PROTACs
Glutathione Peroxidase
Ferroptosis
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Cancer
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NC-R17 is a PROTAC-class, non-covalent GPX4 degrader based on RSL3, involved in ferroptosis. NC-R17 has antitumor activity and is used for non-covalent GPX4 PROTAC design . NC-R17 consists of a target protein ligand (red part) Demethyl-RSL3 (HY-135832); an E3 ubiquitin ligase ligand (blue part) Lenalidomide (HY-A0003) and a PROTAC linker (black part) (HY-169376). E3 ubiquitin ligase and linker can form Lenalidomide-C13-piperazine-Boc (HY-169377); the active control for the target protein ligand is RSL3-4-Me (HY-169375).
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- HY-130988
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GDC-0068-NH2; RG7440-NH2
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Ligands for Target Protein for PROTAC
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Cancer
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Ipatasertib-NH2 (GDC-0068-NH2;RG7440-NH2) is a ligand for target protein AKT for PROTAC (INY-03-041). INY-03-041 is composed of Ipatasertib-NH2, a ten-hydrocarbon linker, and a CRBN ligand Lenalidomide for E3 ubiquitin ligase .
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- HY-129603
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STAT
Ligands for Target Protein for PROTAC
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Cancer
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SI-109 is a potent STAT3 SH2 domain inhibitor (Ki=9 nM) with antitumor activity. SI-109 effectively inhibits the transcriptional activity of STAT3 (IC50=3 μM). SI-109 and an analog of CRBN ligand lenalidomide have been used to design PROTAC STAT3 degrader SD-36 .
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- HY-154984
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Histone Acetyltransferase
PROTACs
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Cancer
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JET-209 is a potent PROTAC CBP/p300 degrader, with DC50 values of 0.05 nM and 0.2 nM for CBP and p300. JET-209 contains Lenalidomide (HY-A0003) (the cereblon ligand), a linker and GNE-207 (HY-120028) (bromodomain Inhibitor). JET-209 is used for cancer research .
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- HY-150797
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QA-68-ZU81
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PROTACs
Epigenetic Reader Domain
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Inflammation/Immunology
Cancer
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QA-68 (QA-68-ZU81) is an effective PROTAC-class BRD9 degrader. QA-68 can inhibit cell cycle progression and cell colony formation. QA-68 has antiproliferative activity against acute myeloid leukemia (AML) cell lines . QA-68 can be formed by a target protein ligand (red part) EA-89 (HY-170314), an E3 ubiquitin ligase ligand (blue part) Lenalidomide-I (HY-131318), and a PROTAC linker (black part) Ethyne-C2-Pip-CO-Pip-Boc (HY-170315). E3 ubiquitin ligase and linker can form Lenalidomide-ethyne-C2-Pip-CO-Pip (HY-170319); the active control for the target protein ligand is EA-89-Succinic acid (HY-170317).
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- HY-157213
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Apoptosis
PROTACs
FLT3
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Cancer
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LWY713 is a PROTAC-class FLT3 degrader (DC50=0.64 nM), which selectively induces FLT3 degradation via cereblon and proteasome-dependent pathways. LWY713 inhibits cell proliferation and induces G0/G1 phase arrest and apoptosis in MV4-11 cells. LWY713 shows effective in vivo antitumor activity in MV4-11 xenograft models . LWY713 consists of a target protein ligand (red part) Gilteritinib (HY-12432), an E3 ubiquitin ligase ligand (blue part) Lenalidomide-F (HY-W039233), and a PROTAC linker (black part) Glycolic acid (HY-W015967). E3 ubiquitin ligase and linker can form Lenalidomide-Glycolic acid (HY-169373); the active control for the target protein ligand is Naproxen Gilteritinib (HY-169374).
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- HY-133120
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PROTACs
Akt
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Cancer
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INY-03-041 is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003, Cereblon ligand). INY-03-041 inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0, 6.8 and 3.5 nM, respectively .
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- HY-133120A
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PROTACs
Akt
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Cancer
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INY-03-041 trihydrochloride is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003, Cereblon ligand). INY-03-041 trihydrochloride inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0, 6.8 and 3.5 nM, respectively .
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- HY-W760183
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Others
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Cancer
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EM12-SO2F is a powerful covalent inhibitor of CRBN through binding at His353. EM12-SO2F is a useful chemical probe to investigate the CRBN. EM12-SO2F inhibits the degradation of IKZF1 by lenalidomide (HY-A0003) in MOLT4 cells
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- HY-145452
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5-Octyl 2-oxopentanedioate
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Others
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Cancer
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5-Octyl-α-ketoglutarate (5-Octyl 2-oxopentanedioate) is a cell-permeable substrate for lysine demethylase. 5-Octyl-α-ketoglutarate is related to protein demethylation, inhibits cell proliferation of wtCRBN expressing cells, and also enhances Lenalidomide (HY-A0003)-induced sensitivity and inhibits myeloma (MM) ) drug resistance of cells. When myeloma (MM) cells undergo glutamine-dependent proliferation, α-ketoglutarate increases glutamine catabolism to promote protein demethylation .
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- HY-161615
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Apoptosis
PROTACs
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Cancer
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PROTAC ATR degrader-2 (Compound 8i) is a PROTAC degrader for ATR, through of . PROTAC ATR degrader-2 degrades ATR in acute myeloid leukemia (AML) cells MV-4-11 and MOLM-13, with DC50 of 22.9 and 34.5 nM. APROTAC ATR degrader-2 induces apoptosis, inhibits proliferations of AML cells. PROTAC ATR degrader-2 exhibits good pharmacokinetics charachers and antitumor efficacy against AML in mouse model. (Pink: ATR ligand (HY-161616); Blue:E3 ligase ligand Lenalidomide (HY-A0003); Black: linker)
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- HY-130985
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PROTAC Linkers
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Cancer
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9-Decyn-1-ol is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs. 9-Decyn-1-ol can be used to conjugate GDC-0068 with Lenalidomide to generate INY-03-041. INY-03-041 is a potent, highly selective and PROTAC-based pan-Akt degrader. INY-03-041 inhibits Akt1, Akt2 and Akt3 with IC50s of 2.0 nM, 6.8 nM and 3.5 nM, respectively . 9-Decyn-1-ol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-129602
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SD-36
5 Publications Verification
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PROTACs
STAT
Apoptosis
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Cancer
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SD-36 is a potent and efficacious STAT3 PROTAC degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase . SD-36 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-131203
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PROTACs
Epigenetic Reader Domain
Apoptosis
c-Myc
Caspase
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Cancer
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PROTAC BRD4 Degrader-6 (compound 32a) is a potent small-molecule BRD4PROTAC degrader with IC50 value of 2.7 nM for BRD4 BD1. PROTAC BRD4 Degrader-6 potently degrades BRD4 protein and inhibits the expression of c-Myc. PROTAC BRD4 Degrader-6 inhibits the proliferation of pancreatic cancer cell line BxPC3 and induces apoptosis. PROTAC BRD4 Degrader-6 can be used for human pancreatic cancer research (Pink:
Mivebresib (HY-100015); Black: linker, Azido-PEG1-CH2CO2H (HY-108369); Blue: Lenalidomide (HY-A0003)) .
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Cat. No. |
Product Name |
Chemical Structure |
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- HY-A0003S
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Lenalidomide-d5 is deuterium labeled Lenalidomide. Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells[1][2].
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- HY-W777286
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rac Lenalidomide-13C5 is a deuterated labeled rac Lenalidomide-13C5 .
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- HY-A0003S2
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Lenalidomide- 13C5, 15N is 15N and 13C labeled Lenalidomide (HY-A0003). Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
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Cat. No. |
Product Name |
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Classification |
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- HY-133139
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Azide
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Lenalidomide-PEG1-azide is a E3 ligase lgand-linker conjugate. Lenalidomide-PEG1-azide incorporates the Lenalidomide based cereblon ligand and a linker.?Lenalidomide-PEG1-azide?can be used to design a PROTAC BRD4 Degrader-2 (HY-133136) . Lenalidomide-PEG1-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-161134
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Azide
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Lenalidomide 4'-PEG2-azide is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide 4'-PEG2-azide can be connected to the ligand for protein by a linker to form PROTAC .
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- HY-161133
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Azide
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Lenalidomide 4'-PEG1-azide (Compound 4g) is a lenalidomide-derived azide. Lenalidomide 4'-PEG1-azide incorporates the Lenalidomide based cereblon ligand and a linker. Lenalidomide 4'-PEG1-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups. .
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- HY-163647
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Azide
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Lenalidomide-COCH-PEG2-azido is a synthesized E3 ligase ligand-linker conjugate that incorporates the Lenalidomide (HY-A0003) based cereblon ligand and a linker. Lenalidomide-COCH-PEG2-azido can be used in the synthesis of PROTAC AKR1C3 degrader-1 (HY-163609) .
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- HY-161131
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Azide
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Lenalidomide 4'-alkyl-C3-azide (compound 4a) is a click chemical modified Lenalidomide (HY-A0003) that can be used to synthesize PROTACs. Lenalidomide is an orally active immunomodulator and a ligand for the ubiquitin E3 ligase cereblon (CRBN). Lenalidomide 4'-alkyl-C3-azide contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition reactions (SPAAC) can also occur with molecules containing DBCO or BCN groups .
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- HY-163964
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Azide
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Lenalidomide-C3-PEG3-N3 is an E3 Ligase Ligand-Linker Conjugate. Lenalidomide-C3-PEG3-N3 can be used to synthesize L18I (HY-163962) .
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- HY-161132
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Azide
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Lenalidomide 4'-alkyl-C5-azide is a functionalized cerebellar ligand for PROTAC development that contains an E3 ligand and an alkyl LC5 ligand with terminal azides that can be coupled to a target protein ligand .
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- HY-159608
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Azide
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PROTAC Cbl-b-IN-1 (compound 64) is a PROTAC targeting Cbl-b. PROTAC Cbl-b-IN-1 is composed of PROTAC target protein ligand Cbl-b-IN-21 (HY-159615), PROTAC Linker Cbz-Pip-2C-Pip-C-Pip (HY-159617) and E3 ubiquitin ligase ligand (3S) Lenalidomide-5-Br (HY-W797329), where the E3 ubiquitin ligase ligand + Linker conjugate is (3S) Lenalidomide-5-Pip-C-Pip-2C-Pip (HY-159618) [1] .
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- HY-130985
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Alkynes
PROTAC Synthesis
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9-Decyn-1-ol is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs. 9-Decyn-1-ol can be used to conjugate GDC-0068 with Lenalidomide to generate INY-03-041. INY-03-041 is a potent, highly selective and PROTAC-based pan-Akt degrader. INY-03-041 inhibits Akt1, Akt2 and Akt3 with IC50s of 2.0 nM, 6.8 nM and 3.5 nM, respectively . 9-Decyn-1-ol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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